Chemical composition, biological activities, and quality standards of hawthorn leaves used in traditional Chinese medicine: a comprehensive review.

Hawthorn leaves also known as crataegi foilum, are a combination of botanical drugs used commonly in Traditional Chinese Medicine. Hawthorn, the plant from which hawthorn leaves are prepared, is distributed in Northeast China, North China, and other regions in China. Hawthorn leaves are known to activate blood circulation and eliminate stasis, invigorating Qi, eliminating turbidity, and reducing the levels of lipids. So far, over a hundred compounds have been isolated from hawthorn leaves, including flavonoids, terpenoids, lignans, organic acids, and nitrogenous compounds. Hawthorn leaves are used for the treatment of hypertension, protecting against ischemic injury, angina, hyperglycemia, hyperlipidemia, and certain other conditions. Several of the currently available clinical preparations also use hawthorn leaves as raw materials, such as Yixintong capsules, Xinan capsules, etc. The present report systematically reviews the chemical composition, biological activities, and quality standards of hawthorn leaves, to provide a scientific basis and reference for detailed research on hawthorn leaves.

Total flavonoids of hawthorn leaves protect spinal motor neurons via promotion of autophagy after spinal cord injury.

The death of spinal motor neurons (SMNs) after spinal cord injury (SCI) is a crucial cause, contributing to a permanent neurological deficit. Total flavonoids of hawthorn leaves (TFHL) have been confirmed to have potentially therapeutic for SCI. Nonetheless, the roles and mechanisms of TFHL in recovering neuromotor function and regenerating axons of SMNs have not been fully elucidated. In this study, TFHL was applied to treat rats with SCI and injured SMNs for 7 days. In vivo experiment, rats with SCI were evaluated by a BBB (Basso-Beattie-Bresnahan) score to assess their motor functional recovery. The morphology, microstructure, apoptosis, Nissl bodies, and autophagy of SMNs in spinal cord tissue were detected by Hematoxylin-eosin (HE) staining, transmission electron microscopy, TUNEL staining, Nissl staining, and immunohistochemistry respectively. In vitro experiment, the co-culture model of SMNs and astrocytes was constructed to simulate the internal environment around SMNs in the spinal cord tissue. The cell morphology, microstructure, axonal regeneration, and autophagy were observed via optical microscope, transmission electron microscopy, and immunofluorescence. The content of neurotrophic factors in the cell culture medium of the co-culture model was detected by ELISA. Moreover, the expression of axon-related and autophagy-related proteins in the spinal cord tissue and SMNs was measured by Western Blot. We demonstrated that TFHL improved the neuromotor function recovery in rats after SCI. We then found that TFHL significantly promoted injured spinal cord tissue repair, reduced apoptosis, and improved the functional status of neurons in spinal cord tissue in vivo. Meanwhile, the cell morphology, microstructure, and axonal regeneration of damaged SMNs also obviously were improved, and the secretion of neurotrophic factors was facilitated after treatment with TFHL in vitro. Further, we revealed that TFHL promoted autophagy and related protein expression in vivo and vitro. Taken together, our study suggested that TFHL might facilitate autophagy and have neuroprotective properties in SMNs to enhance the recovery of neuromotor function of rats with SCI.

Exploring the Mechanism of Hawthorn Leaves Against Coronary Heart Disease Using Network Pharmacology and Molecular Docking.

Hawthorn leaves, which is a traditional Chinese medicine (TCM), has been used for treating coronary heart disease (CHD) for a long time in China. But the limited understanding of the main active components and molecular mechanisms of this traditional medicine has restricted its application and further research. The active compounds of hawthorn leaves were obtained from TCMSP database and SymMap database. The targets of it were predicted based on TCMSP, PubChem, Swiss Target Prediction, and SymMap database. The putative targets of CHD were gathered from multi-sources databases including the Online Mendelian Inheritance in Man (OMIM) database, the DrugBank database, the GeneCards database and the DisGeNet database. Network topology analysis, GO and KEGG pathway enrichment analyses were performed to select the key targets and pathways. Molecular docking was performed to demonstrate the binding capacity of the key compounds to the predicted targets. Furthermore, RAW264.7 cells stimulated by lipopolysaccharides (LPS) were treated with three effective compounds of hawthorn leaves to assess reliability of prediction. Quercetin, isorhamnetin and kaempferol were main active compounds in hawthorn leaves. Forty four candidate therapeutic targets were identified to be involved in protection of hawthorn leaves against CHD. Additionally, the effective compounds of it had good binding affinities to PTGS2, EGFR, and MMP2. Enrichment analyses suggested that immune inflammation related biological processes and pathways were possibly the potential mechanism. Besides, we found that three predicted effective compounds of hawthorn leaves decreased protein expression of PTGS2, MMP2, MMP9, IL6, IL1B, TNFα and inhibited activation of macrophage. In summary, the present study demonstrates that quercetin, kaempferol and isorhamnetin are proved to be the main effective compounds of hawthorn leaves in treatment of CHD, possibly by suppressing expression of PTGS2, MMP2, MMP9, inflammatory cytokines and macrophages viability. This study provides a new understanding of the active components and mechanisms of hawthorn leaves treating CHD from the perspective of network pharmacology.

Quality analysis of hawthorn leaves (the leaves of Crataegus pinnatifida Bge. var major N.E.Br) in different harvest time.

INTRODUCTION: Harvest time plays an important role on the quality of medicinal plants. The leaves of Crataegus pinnatifida Bge. var major N.E.Br (hawthorn leaves) could be harvested in summer and autumn according to the Pharmacopoeia of the People's Republic of China (Pharmacopoeia). However, little is known about the difference of the chemical constituents in hawthorn leaves with the harvest seasonal variations. OBJECTIVE: The chemical constituents of hawthorn leaves in different months were comprehensively analysed to determine the best harvest time. METHODS: Initially, the chemical information of the hawthorn leaves were obtained by ultra-high-performance liquid chromatography and quadrupole time-of-flight mass spectrometry (UHPLC-Q-TOF-MS). Subsequently, principal component analysis (PCA) was applied to compare the chemical compositions of hawthorn leaves harvested in different months. Then, an absolute quantitation method was established using high-performance liquid chromatography-charged aerosol detector (HPLC-CAD) to determine the contents of five compounds and clarify the changes of these components with the harvest seasonal variations. Meanwhile, a semi-quantitative method by integrating HPLC-CAD with inverse gradient compensation was also established and verified. RESULTS: Fifty-eight compounds were identified through UHPLC-Q-TOF-MS. PCA revealed that the harvest season of hawthorn leaves had a significant effect on the chemical compositions. The contents of five components were relatively high in autumn. Other four main components without reference standards were further analysed through the semi-quantitative method, which also showed a high content in autumn. CONCLUSIONS: This work emphasised the effect of harvest time on the chemical constituents of hawthorn leaves and autumn is recommended to ensure the quality.

Dietary hawthorn-leaves flavonoids improves ovarian function and liver lipid metabolism in aged breeder hens.

Hawthorn-leaves flavonoids (HF), extracted from hawthorn leaves, were reported to exert antioxidant, anti-inflammatory and hypolipidemic properties. The aim of our study was to investigate the effects of dietary HF on the reproduction performance and liver lipid metabolism of aged breeder hens. A total of 270 aged Qiling breeder hens (60-wk-old) were randomly divided into 3 treatments: 1) basic corn-soybean diet (CON); 2) basic corn-soybean diet supplemented with 30 mg/kg HF (LHF); 3) basic corn-soybean diet supplemented with 60 mg/kg HF (HHF). The results showed that supplemented HF significantly improved the egg-laying rate and hatching rate of aged breeder hens (P < 0.05). HF treatment reduced the serum TG, T-CHO and L-LDL levels (P < 0.05), and upregulated the mRNA expressions of ESR1, ESR2, VTGⅡ, ApoB, and ApoVI in the liver (P < 0.05). Serum estrogen levels in HF treated groups were elevated compared with the CON group (P < 0.05). In the HHF group, the number of the primordial follicles was higher in comparison with the CON group (P < 0.05). Furthermore, dietary supplementation with HF improved the activity of antioxidant enzymes (T-AOC, GSH-Pχ) (P < 0.05), following with the reversed ovarian apoptosis and morphological damage. In addition, 60 mg/kg dietary HF upregulated the protein expression of PCNA and Nrf2 in the ovary (P < 0.05). In summary, dietary supplementation with HF could improve the reproduction performance through regulating liver lipid metabolism and improving ovarian function in aged breeder hens.

[Terpenoids from leaves of Chinese hawthorn].

Fifteen compounds were isolated from the 70% EtOH extract of leaves of Chinese hawthorn(Crataegus pinnatifida var. major) by various purification steps, and their structures were determined as 2α,3α,12ß,19α,-tetrahydroxyursan-13ß,28-olide(1),euscaphic acid(2), tormentic acid(3), ursolic acid(4), pomolic acid(5), corosolic acid(6), maslinic acid(7), linalyl rutinoside(8),(Z)-3-hexenyl ß-D-glucoside(9),(3S, 6S)-cis-linalool-3,7-oxide-ß-D-glucopyranoside(10), pisumionoside(11), icariside B6(12), byzantionoside B(13),(6R,7E,9R)-9-Hydroxy-4,7-megastigmadien-3-one 9-O-ß-D-glucopyranoside(14) and(6S,7E,9R)-6,9-dihydroxy-4,7-megastigmadien-3-one 9-O-ß-D-glucopyranoside(15) mainly based on the mass spectrum(MS) and nuclear magnetic resonance(NMR) spectroscopic techniques, of which compound 1 was a new pentacyclic triterpene, and compounds 2, 5, 6, 8, 10, 13 and 15 were isolated form this plant for the first time.

Total flavonoids of hawthorn leaves promote motor function recovery via inhibition of apoptosis after spinal cord injury.

Flavonoids have been reported to have therapeutic potential for spinal cord injury. Hawthorn leaves have abundant content and species of total flavonoids, and studies of the effects of the total flavonoids of hawthorn leaves on spinal cord injury have not been published in or outside China. Therefore, Sprague-Dawley rats were used to establish a spinal cord injury model by Allen's method. Rats were intraperitoneally injected with 0.2 mL of different concentrations of total flavonoids of hawthorn leaves (5, 10, and 20 mg/kg) after spinal cord injury. Injections were administered once every 6 hours, three times a day, for 14 days. After treatment with various concentrations of total flavonoids of hawthorn leaves, the Basso, Beattie, and Bresnahan scores and histological staining indicated decreases in the lesion cavity and number of apoptotic cells of the injured spinal cord tissue; the morphological arrangement of the myelin sheath and nerve cells tended to be regular; and the Nissl bodies in neurons increased. The Basso, Beattie, and Bresnahan scores of treated spinal cord injury rats were increased. Western blot assays showed that the expression levels of pro-apoptotic Bax and cleaved caspase-3 were decreased, but the expression level of the anti-apoptotic Bcl-2 protein was increased. The improvement of the above physiological indicators showed a dose-dependent relationship with the concentration of total flavonoids of hawthorn leaves. The above findings confirm that total flavonoids of hawthorn leaves can reduce apoptosis and exert neuroprotective effects to promote the recovery of the motor function of rats with spinal cord injury. This study was approved by the Ethics Committee of the Guangxi Medical University of China (approval No. 201810042) in October 2018.

Terpenoids from leaves of Chinese hawthorn / 中国中药杂志

Fifteen compounds were isolated from the 70% EtOH extract of leaves of Chinese hawthorn(Crataegus pinnatifida var. major) by various purification steps, and their structures were determined as 2α,3α,12β,19α,-tetrahydroxyursan-13β,28-olide(1),euscaphic acid(2), tormentic acid(3), ursolic acid(4), pomolic acid(5), corosolic acid(6), maslinic acid(7), linalyl rutinoside(8),(Z)-3-hexenyl β-D-glucoside(9),(3S, 6S)-cis-linalool-3,7-oxide-β-D-glucopyranoside(10), pisumionoside(11), icariside B6(12), byzantionoside B(13),(6R,7E,9R)-9-Hydroxy-4,7-megastigmadien-3-one 9-O-β-D-glucopyranoside(14) and(6S,7E,9R)-6,9-dihydroxy-4,7-megastigmadien-3-one 9-O-β-D-glucopyranoside(15) mainly based on the mass spectrum(MS) and nuclear magnetic resonance(NMR) spectroscopic techniques, of which compound 1 was a new pentacyclic triterpene, and compounds 2, 5, 6, 8, 10, 13 and 15 were isolated form this plant for the first time.

Hawthorne leaf flavonoids prevent oxidative stress injury of renal tissues in rats with diabetic kidney disease by regulating the p38 MAPK signaling pathway.

Objectives: Diabetic kidney disease (DKD) is the primary microvascular complication of diabetes. The incidence rate of DKD has increased worldwide, and DKD has become one of the most important causes of end-stage renal disease. In this study, we aimed to investigate the effects of hawthorn leaf flavonoids (HLF) on oxidative stress injury of renal tissue in DKD rats, and elucidate their mechanism(s) of action. Methods: A total of 35 male Sprague Dawley rats were randomly divided into the control group (CON group) and model group. Rats in the model group were fed a diet containing high sugar and fat and were injected with streptozotocin (STZ) into the abdominal cavity to induce diabetes. Diabetic rats that showed >50% increase in 24 h urine volume and >30 mg of 24 h urine protein excretion were selected as DKD model rats. After DKD models were successfully established, model rats were randomly divided into the diabetic kidney disease group (DKD group), irbesartan group (IRB group), and hawthorn leaf flavonoids group (HLF group). All rats were sacrificed at 12 weeks (w) after DKD models were established. Body weight and 24 h urinary protein levels were measured at 4 w, 8 w, and 12 w, respectively. Blood was collected to measure the levels of urea nitrogen, creatinine, triglyceride, nitric oxide, malondialdehyde, and superoxide dismutase. Pathologic changes in renal tissue were examined by hematoxylin and eosin (H&E) and Masson staining. Protein expression of p38MAPK and p-p38MAPK was determined by immunohistochemistry. Results: Our data showed that HLFs improved the general condition and body weight, and reduced the levels of urinary protein in model rats. Rats in the DKD group had more serious pathological damage in the kidney when compared to rats in the HLFs group. In addition, rats in the HLF group had significantly lower levels of urea nitrogen, creatinine, triglyceride, and malondialdehyde, and significantly higher levels of nitric oxide and superoxide dismutase than rats in the DKD group. Furthermore, p38MAPK and p-p38MAPK protein levels were significantly higher in rats in the DKD group compared to rats in the HLF group. Conclusions: HLFs have a protective effect against DKD in rats. The underlying mechanism may involve the reduction of oxidative stress by inactivation of the p38MAPK signaling pathway in renal tissues.

Experimental study on inhibitory effect of hawthorn leaves flavonoids on human glioblastoma U87 cells / 中国药理学通报

Aim To explore the inhibitory effect of hawthorn leaves flavonoids (HLF) on human glioblastoma U87 cells. Methods U87 cells were cultured in vitro. The concentration of HLF was 25, 50, 100 mg . L¹ as drug concentration. The effects of HLF on the proliferation, migration, invasion and adhesion of U87 cells were detected by CCK-8 assay, scratch assay, Transwell assay and adhesion assay, and clone forming ability was detected by cell clonogenic assay. Results HLF inhibited the proliferation, migration, invasion and adhesion of U87 cells in a concentration-dependent manner, and the difference was statistically significant compared with control group (P < 0. 05). When HLF reached 50 mg . L¹ the inhibition of tumor growth was the most significant. Conclusion HLF has a certain inhibitory effect on glioma U87 cells.

[Key physical parameters of hawthorn leaf granules by stepwise regression analysis method].

The purpose of this study was to investigate the effect of key physical properties of hawthorn leaf granule on its dissolution behavior. Hawthorn leaves extract was utilized as a model drug. The extract was mixed with microcrystalline cellulose or starch with the same ratio by using different methods. Appropriate amount of lubricant and disintegrating agent was added into part of the mixed powder, and then the granules were prepared by using extrusion granulation and high shear granulation. The granules dissolution behavior was evaluated by using equilibrium dissolution quantity and dissolution rate constant of the hypericin as the indicators. Then the effect of physical properties on dissolution behavior was analyzed through the stepwise regression analysis method. The equilibrium dissolution quantity of hypericin and adsorption heat constant in hawthorn leaves were positively correlated with the monolayer adsorption capacity and negatively correlated with the moisture absorption rate constant. The dissolution rate constants were decreased with the increase of Hausner rate, monolayer adsorption capacity and adsorption heat constant, and were increased with the increase of Carr index and specific surface area. Adsorption heat constant, monolayer adsorption capacity, moisture absorption rate constant, Carr index and specific surface area were the key physical properties of hawthorn leaf granule to affect its dissolution behavior.

Research on equilibrium solubility and apparent oil/water partition coefficient of flavonoids components in hawthorn leaves by similarity analysis / 中草药

Objective To study the equilibrium solubility and oil/water partition coefficient of Hawthorn leaves flavonoids (HLF) components, and compare their similarity, to lay the foundation for the characterization of the overall water soluble and fat soluble HLF components. Methods Taking HLF components as model drug, rutin, quercetin, and hyperin as representative components. The HPLC method was used to determine the equilibrium solubility and apparent oil/water distribution coefficient (Papp) of the components at different pH values and water. The similarity was evaluated by the vector cosine method (cosines) and Grubbs method (Grubbs). Chromatographic conditions: The chromatographic column was Zorbax Eclipse Plus C18 column (250 mm × 4.6 mm, 5 μm), and the flow phase was acetonitrile (A) - 0.4% phosphate solution (B). The gradient elution program was 0—10 min (80% B), 10—11 min (80%—60% B), 11—20 min (60% B), 20—21 min (60%—80% B), and 21—25 min (80% B); The detection wavelength was 360 nm; The volume flow was 0.8 mL/min; The column temperature was 40 ℃. Results The equilibrium solubility and Papp of rutin, quercetin, hyperin were similar in different pH buffer solution and water. The solubility value of lutin, quercetin, and hyperoside in thebuffer solution of different pH were 0.998, 0.988, and 0.987, respectively. The cosine value of the apparent oil-water distribution coefficient was 0.976, 0.981, and 0.978, respectively. The cosine value was greater than 0.9. The Grubbs value of equilibrium solubility of lutin, quercetin and hyperoside were 1.057, 1.083, 1.124, 1.117, 1.022, 1.030, 1.082, and 1.112, respectively. The Grubbs values of the apparent oil-water distribution coefficient were 1.125, 1.107, 1.079, 1.034, 1.041, 1.037, 1.129, and 1.128. The results of Grubbs were less than G critical value of 1.153, and the similarity was good. Conclusion The similarity analysis reflects that the degree of dispersion of components objectively, which could increase the science of components evaluation and provide the basis for the formulation design of components of traditional Chinese medicine.

Key physical parameters of hawthorn leaf granules by stepwise regression analysis method / 中国中药杂志

The purpose of this study was to investigate the effect of key physical properties of hawthorn leaf granule on its dissolution behavior. Hawthorn leaves extract was utilized as a model drug. The extract was mixed with microcrystalline cellulose or starch with the same ratio by using different methods. Appropriate amount of lubricant and disintegrating agent was added into part of the mixed powder, and then the granules were prepared by using extrusion granulation and high shear granulation. The granules dissolution behavior was evaluated by using equilibrium dissolution quantity and dissolution rate constant of the hypericin as the indicators. Then the effect of physical properties on dissolution behavior was analyzed through the stepwise regression analysis method. The equilibrium dissolution quantity of hypericin and adsorption heat constant in hawthorn leaves were positively correlated with the monolayer adsorption capacity and negatively correlated with the moisture absorption rate constant. The dissolution rate constants were decreased with the increase of Hausner rate, monolayer adsorption capacity and adsorption heat constant, and were increased with the increase of Carr index and specific surface area. Adsorption heat constant, monolayer adsorption capacity, moisture absorption rate constant, Carr index and specific surface area were the key physical properties of hawthorn leaf granule to affect its dissolution behavior.

Separation of vitexin-4″-O-glucoside and vitexin-2″-O-rhamnoside from hawthorn leaves extracts using macroporous resins.

Vitexin-4″-O-glucoside and vitexin-2″-O-rhamnoside are the major flavonoids of hawthorn leaves. In this work, the adsorption and desorption characteristics of vitexin-4″-O-glucoside and vitexin-2″-O-rhamnoside on seven macroporous resins were evaluated. Among the tested resins, the HPD-400 resin showed the best adsorption and desorption capacities. Adsorption isotherms were constructed for the HPD-400 resin and well fitted to Langmuir and Freundlich models. Dynamic adsorption and desorption tests were performed on column packed with the HPD-400 resin to optimize the chromatographic parameters. After one run treatment with the HPD-400 resin, the contents of vitexin-4″-O-glucoside and vitexin-2″-O-rhamnoside in the product were increased 8.44-fold and 8.43-fold from 0.720% and 2.63% to 6.08% and 22.2% with recovery yields of 79.1% and 81.2%, respectively. These results show that the developed method is a promising basis for the large-scale purification of vitexin-4″-O-glucoside and vitexin-2″-O-rhamnoside from hawthorn leaves and other plant materials.

Simultaneous Determination of Four Flavonoids in Extract of Hawthorn Leaves by Microemulsion Liquid Chromatography / 分析化学

A novel system was developed for the rapid determination of vitexin, vitexin-2″-O-rhamnoside, rutin, and hyperoside in the extract of hawthorn(Crataegus pinnatifida Bge.) leaves with microemulsion liquid chromatography(MELC). The effect on the chromatography of varying the operating paramers was studied. The optimized MELC system with microemulsion was consisting of 1.0%(w/w) brij35-1.1%(w/w) n-butanol-0.1%(w/w) n-octanol-0.3%(v/v) triethylamine, the pH was adjusted to 2.5 with phosphoric acid. The type and concentration of surfactant, types of oil phase, the pH and triethylamine as the organic additive in microemulsion played an important role for separation of four flavonoids. MELC analysis was performed on a Venusil ASB C_(18) analytical column (150 mm× 4.6 mm, i.d., 5 μm). The flow rate was set at 0.8 mL/min and the eluent was detected at 340 nm for the four flavonoids. The calibration curves of the four flavonoids are linear(r>0.9995) over the concentration range of 0.95-140.0 mg/L. The mean recoveries are 98.6% to 101.6%. The results indicate that the optimized method was successfully applied to the analysis of four important flavonoids in the extract of hawthorn leaves.

Comparative analysis of ursolic acid in Hawthorn leaves by HPLC / 中成药

AIM: To develop a simple HPLC for the determination of ursolic acid in Hawthorn leaves, and to compare ursolic acid content in Hawthorn leaves of different species, locations and growth stages, so as to supply some evidences for the exploitation and utilization of Hawthorn leaves reasonably. METHODS: By high-performance liquid chromatography method. Lichrospher C18 column (250 ×4.6 mm I. D. 5 μm); mobile phase, acetonitrile-water-orthophosphoric acid (85: 14.95: 0.05) with a flow-rate of 1.00 ml/min; column temperature at 30 ℃; injection volume, 5μl; UV detector at 210 nm. RESULTS: The detection limit (S/N=3) was less than 4. 024 μg/ml and the limit of quantification( S/N =10) was less than 12.05 μg/ml. The calibration curve showed good linear regression(r =0. 9999) within measurement ranges( 16.09 - 1030 μg/ml). The intra-day and interday variation were 0.71% and 6. 15%, respectively. The recoveries at low to high concentration were 89%-105%. Under these conditions, the ursolic acid content in different Hawthorn leaves were determined: 1.90%-1.95% in C. scabrifolia (Franch.) Rehd, 1.00%-1.45% in C. cuneata Sieb. & Zucc, 0.45%-0.65% in C.pinnatifida Bge. var. major N. E. Br.; In differnet growth stages of C. pinnatifida Bge. var. major N. E. Br. , the young leaves contain higher content of ursolic acid. CONCLUSION: The method is successfully applied to quantify ursolic acid in Hawthorn leaves. And the ursolic acid contents in Hawthorn leaves of differnent species are very different; C. scabrifolia (Franch.) Rehd contains the highest ursolic acid content in them. However, there is a little difference among different locations and growth stages for same species.

Self-microemulsifying drug delivery system of flavonoids in hawthorn leaves / 中草药

Objective To develop the formulation of self-microemulsifying drug delivery system for hawthorn leaves flavonoids (HAW-SMEDDS). Methods The optimum formulations of oil phase, surfactant, and assistant surfactant for HAW-SMEDDS were screened by solubility test, compatibility test, and pseudo-ternary phase diagrams, with the time of formulating microemulsion, the consequence of visual examination, and particle size as indexes. The dissolution of HAW-SMEDDS was measured, taking the commercial tablet Yixintong Tablet as reference. Results The optimum self-microemulsifying drug delivery system was composed of Labrasol (35%), Transcutol P (10%). The particle diameter was (39.5?5.4) nm, the time of self-microemulsifying was less than 1 min. The percent of accumulated dissolution of hawthorn leaves flavonoids in SMEDDS in distilled water was up to 70% at 10 min, while that in the Yixintong Tablet was less than 50% at 60 min. Conclusion The formulation of HAW-SMEDDS preparation could meet the request of the design. It could provide the reference for the new dosage form.

In situ rat intestinal absorption of hawthorn leaves flavonoids / 中成药

0.05).But the P_ eff values were significantly increased in the presence of P-glycoportein(P-gp)inhibitor,verapamil or digoxin.CONCLUSION:Rhamnosylvitexin can be classified into high penetrating drug.Passive diffusion dominates the absorptive transport behavior of rhamnosylvitexin in HLF.There is not a preferential absorption zone in the intestine for rhamnosylvitexin.The absorption and secretion of rhamnosylvitexin in HLF are mediated by the efflux transport system,P-gp.

HPLC fingerprint chromatogram of leaves of Hawthorn / 中成药

AIM: To establish HPLC fingerprint chromatogram of leaves of Hawthorn and to evaluate the constituents and to provide the basis for identification. METHODS: Leaves of Hawthorn come from 10 production places were analysed to gain its contents,such as Vitexin,Hyperoside,2″-O-Rhamnosylvitexin,Rutin,4-O-Rhamnosylrutin,Chlorogenic acid,Quercetin 3-O-?-glucoside,4-O-Glucosylvitexiu,and internal reference selected Chlorogenic acid. RESULTS: The different leaves of Hawthorn showed different HPLC chromatogram. CONCLUSION: HPLC chromatogram can be used to distinguish the leaves of different species of Hawthorn and the content of the main characteristic components are various as production places vary.